公开(公告)号：US20240351986A1

公开(公告)日：2024-10-24

申请号：US18683623

申请日：2022-07-26

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Youhong HU ,  Yi CHEN ,  Zhicheng XIE ,  Jian DING ,  Xin LI ,  Yanfen FANG ,  Qianqian SHEN

IPC: C07D213/75 ,  A61K31/4418 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4985 ,  A61K31/505 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/55 ,  A61P35/00 ,  C07D239/42 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D487/04 ,  C07D498/04

CPC classification number: C07D213/75 ,  A61K31/4418 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4985 ,  A61K31/505 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/55 ,  A61P35/00 ,  C07D239/42 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D487/04 ,  C07D498/04

Abstract: The present invention relates to a urea compound containing 2-heteroaromatic ring substitution represented by formula (I), its enantiomers, diastereomers, racemates or mixtures thereof, or pharmaceutically acceptable salts thereof, solvate, metabolite or prodrug. The compound of formula (I) of the present invention has inhibitory activity against CDK9, and representative compounds have significant anti-tumor activity against CDK9 high-expressing tumor cells. Representative compounds have plasma stability and low clearance.

公开(公告)号：US20200172502A1

公开(公告)日：2020-06-04

申请号：US16623297

申请日：2018-05-31

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES ,  FUKANG (SHANGHAI) HEALTH TECHNOLOGY CO., LTD.

Inventor： Chunhao YANG ,  Zehong MIAO ,  Cun TAN ,  Xiajuan HUAN ,  Jian DING ,  Yi CHEN

IPC: C07D307/84

Abstract: Disclosed are a 2-[4-(methylaminomethyl)phenyl]-5-fluoro-benzofuran-7-carboxamide hydrochloride polymorph, a preparation method therefor and an application thereof. Specifically, disclosed are three crystalline forms, i.e., crystalline forms A, B, and C, of 2-[4-(methylaminomethyl)phenyl]-5-fluoro-benzofuran-7-carboxamide hydrochloride (formula I), preparation methods for the three crystalline forms, and use of the three crystalline forms in preparation of drugs.

公开(公告)号：US20200247781A1

公开(公告)日：2020-08-06

申请号：US16652148

申请日：2018-09-29

Applicant: SHANGHAI HAIHE PHARMACEUTICAL CO., LTD. ,  SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Lei LI ,  Meiyu GENG ,  Ying HUANG ,  Jian DING ,  Qiong ZHANG ,  Min HUANG ,  Shuai TANG ,  Ning SHEN ,  Yi CHEN

IPC: C07D401/14 ,  C07D405/14 ,  C07D403/14

Abstract: The invention relates to a compound of formula (I): wherein variables are as defined in the specification. The compound is an inhibitor of an ERK kinase, e.g. ERK1 and/or ERK2 kinase. The invention also relates to the use of the compound and a method for preparing the compound, and a pharmaceutical composition containing the compound.

公开(公告)号：US20200157110A1

公开(公告)日：2020-05-21

申请号：US16626254

申请日：2018-06-22

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Chunhao YANG ,  Linghua MENG ,  Haoyue XIANG ,  Jing LI ,  Xi ZHANG ,  Xiang WANG ,  Cun TAN ,  Qian HE ,  Jian DING ,  Yi CHEN

IPC: C07D487/04 ,  C07D519/00

Abstract: The present disclosure relates to 7-substituted pyrrolo[2,1-f][1,2,4]triazine compounds or pharmaceutically acceptable salts thereof, and preparation methods and uses thereof. These compounds show good PI3K inhibitory activity, can effectively inhibit the activity of PI3K kinase, and has significant enhancement and improvement of pharmacokinetic properties, such as bioavailability, due to the introduction of the 7-position group; furthermore, the compounds of the present disclosure exhibit an unpredictable high selectivity and strong inhibitory activity on PI3Kδ, and thus these compounds can be used for treating diseases related to PI3K pathway, especially for anti-cancer or for the treatment of tumors, leukemias and autoimmune diseases. After further optimizing and screening, the compounds are expected to be developed into a new type of anti-tumor drugs.

公开(公告)号：US20190211010A1

公开(公告)日：2019-07-11

申请号：US16331090

申请日：2017-09-06

Applicant: SHANGHAI HAIHE PHARMACEUTICAL CO., LTD. ,  SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Xuxing CHEN ,  Meiyu GENG ,  Lei JIANG ,  Yi CHEN ,  Jianhua CAO ,  Qingyun JIANG ,  Qianqian SHEN ,  Jian DING ,  Yucai YAO ,  Zhao ZHAO ,  Yuanfang XIONG

IPC: C07D471/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61P35/00 ,  A61P37/06 ,  C07D519/00

Abstract: The present invention provides a pyrido five-element aromatic ring compound, and a preparation method therefor and a use thereof. The compound provided in the present invention has an inhibitory effect on wild-type and/or mutant EZH2, and is well positioned to become a novel anti-tumor drug or a drug for the treatment of autoimmune diseases.

公开(公告)号：US20190211005A1

公开(公告)日：2019-07-11

申请号：US16329336

申请日：2017-08-24

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Fajun NAN ,  Jia LI ,  Jian DING ,  Meiyu GENG ,  Yangming ZHANG ,  Yi CHEN ,  Yubo ZHOU ,  Chaojun GONG ,  Mingbo SU ,  Anhui GAO

IPC: C07D417/04 ,  A61P35/02

Abstract: The invention describes an aryl-2,2′-tandem bisthiazole compound and a preparation method and the use thereof. In particular, disclosed in the present invention are an aryl-2,2′-tandem bisthiazole compound with the structure as shown in general formula I and the preparation method thereof and use thereof as a histone deacetylase inhibitor in the preparation of antitumor drugs.